Microemulsions formed by PPG-5-CETETH-20 at low concentrations for transdermal delivery of nifedipine
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Colloids and Surfaces B: Biointerfaces
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Nifedipine is a potent anti-hypertensive, which is poorly orally bioavailable on account of first-pass metabolism,
short half-life, and low water solubility. This study aimed to develop a microemulsified system with low surfactant
concentration and to evaluate the influence of microemulsion (ME) phase behavior on skin permeation of
nifedipine, as drug model. Thereafter, MEs were obtained using PPG-5-CETETH-20, oleic acid, and phosphate
buffer at pH 5.0. The selected MEs were isotropic, with droplet diameters less than 10 nm, polydispersity index
< 0.25, and pH between 5.0 and 5.2. MEs presented low viscosity and Newtonian behavior. SAXS results
confirmed bicontinuous and oil-in-water (o/w) MEs formation. The presence of the drug promoted only very
slight modifications in the ME structure. The MEs presented ability to deliver nifedipine via the transdermal
route when in comparison with the control. Nevertheless, the skin permeated and retained amounts from the o/w
and bicontinuous formulations did not differ significantly. The ATR-FTIR demonstrated that both formulations
promoted fluidization and disorganization of lipids and increased the drug diffusion and partition coefficients in
the skin. In conclusion, PPG-5-CETETH-20 MEs obtained proved to be effective skin permeation enhancers,
acting by rising the coefficients of partition and diffusion of the nifedipine in the skin.
Como referenciar
ARAUJO, GUILHERME R.S. de; MACIEIRA, GIVALDA M. da C.; OLIVEIRA, DAYANE X. de; MATOS, SAULO S.; SANTOS, QUESIA N. dos; OTUBO, LARISSA; ARAUJO, ADRIANO A. de S.; DUARTE, MARCELO C.; LIRA, ANA A.M.; NUNES, ROGERIA de S.; SARMENTO, VICTOR H.V. Microemulsions formed by PPG-5-CETETH-20 at low concentrations for transdermal delivery of nifedipine: structural and in vitro study. Colloids and Surfaces B: Biointerfaces, v. 214, p. 1-9, 2022. DOI: 10.1016/j.colsurfb.2022.112474. Disponível em: http://repositorio.ipen.br/handle/123456789/33167. Acesso em: 20 Mar 2026.
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